Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10730519 | Applied Radiation and Isotopes | 2009 | 6 Pages |
Abstract
Alkylating agents have been shown to be very promising for the radiolabelling of oligonucleotides with fluorine-18. In this report we describe the fully automated synthesis of 2-bromo-N-[3-(2-[18F]fluoropyridin-3-yloxy)propyl]acetamide ([18F]FPyBrA) utilizing a modular synthesis unit. Reaction conditions for the coupling of this pyridine-based alkylating agent at the 5Ⲡend of a fully phosphorothioated random 20-mer DNA sequence were optimized to achieve very high radiochemical yields (>90%) and a maximum specific activity of 5-6 GBq/μmoL. The potential for rapid purification by solid phase extraction without need of chromatographic isolation of the radiolabelled oligonucleotide presents an overall benefit for the application of oligonucleotides in preclinical studies and potential clinical applications.
Related Topics
Physical Sciences and Engineering
Physics and Astronomy
Radiation
Authors
Elisabeth von Guggenberg, Jayden A. Sader, John S. Wilson, Soraya Shahhosseini, Ingrid Koslowsky, Frank Wuest, John R. Mercer,